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class="vector-toc-list"> <li id="toc-Ligand_gated_ion_channel_inverse_agonists" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Ligand_gated_ion_channel_inverse_agonists"> <div class="vector-toc-text"> <span class="vector-toc-numb">1.1</span> <span>Ligand gated ion channel inverse agonists</span> </div> </a> <ul id="toc-Ligand_gated_ion_channel_inverse_agonists-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-G_protein-coupled_receptor_inverse_agonists" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#G_protein-coupled_receptor_inverse_agonists"> <div class="vector-toc-text"> <span class="vector-toc-numb">1.2</span> <span>G protein-coupled receptor inverse agonists</span> </div> </a> <ul id="toc-G_protein-coupled_receptor_inverse_agonists-sublist" class="vector-toc-list"> </ul> </li> </ul> </li> <li id="toc-Mechanisms_of_action" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Mechanisms_of_action"> <div class="vector-toc-text"> <span class="vector-toc-numb">2</span> <span>Mechanisms of action</span> </div> </a> <ul id="toc-Mechanisms_of_action-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-See_also" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#See_also"> <div class="vector-toc-text"> <span class="vector-toc-numb">3</span> <span>See also</span> </div> </a> <ul id="toc-See_also-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-References" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#References"> <div class="vector-toc-text"> <span class="vector-toc-numb">4</span> <span>References</span> </div> </a> <ul id="toc-References-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-External_links" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a 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Available in 18 languages" > <label id="p-lang-btn-label" for="p-lang-btn-checkbox" class="vector-dropdown-label cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--action-progressive mw-portlet-lang-heading-18" aria-hidden="true" ><span class="vector-icon mw-ui-icon-language-progressive mw-ui-icon-wikimedia-language-progressive"></span> <span class="vector-dropdown-label-text">18 languages</span> </label> <div class="vector-dropdown-content"> <div class="vector-menu-content"> <ul class="vector-menu-content-list"> <li class="interlanguage-link interwiki-ar mw-list-item"><a href="https://ar.wikipedia.org/wiki/%D9%86%D8%A7%D9%87%D8%B6_%D8%B9%D9%83%D8%B3%D9%8A" title="ناهض عكسي – Arabic" lang="ar" hreflang="ar" data-title="ناهض عكسي" data-language-autonym="العربية" data-language-local-name="Arabic" class="interlanguage-link-target"><span>العربية</span></a></li><li class="interlanguage-link interwiki-de mw-list-item"><a href="https://de.wikipedia.org/wiki/Inverser_Agonist" title="Inverser Agonist – German" lang="de" hreflang="de" data-title="Inverser Agonist" data-language-autonym="Deutsch" data-language-local-name="German" class="interlanguage-link-target"><span>Deutsch</span></a></li><li class="interlanguage-link interwiki-es mw-list-item"><a href="https://es.wikipedia.org/wiki/Agonista_inverso" title="Agonista inverso – Spanish" lang="es" hreflang="es" data-title="Agonista inverso" data-language-autonym="Español" data-language-local-name="Spanish" class="interlanguage-link-target"><span>Español</span></a></li><li class="interlanguage-link interwiki-fa mw-list-item"><a href="https://fa.wikipedia.org/wiki/%D8%A2%DA%AF%D9%88%D9%86%DB%8C%D8%B3%D8%AA_%D9%85%D8%B9%DA%A9%D9%88%D8%B3" title="آگونیست معکوس – Persian" lang="fa" hreflang="fa" data-title="آگونیست معکوس" data-language-autonym="فارسی" data-language-local-name="Persian" class="interlanguage-link-target"><span>فارسی</span></a></li><li class="interlanguage-link interwiki-fr mw-list-item"><a href="https://fr.wikipedia.org/wiki/Agoniste_inverse" title="Agoniste inverse – French" lang="fr" hreflang="fr" data-title="Agoniste inverse" data-language-autonym="Français" data-language-local-name="French" class="interlanguage-link-target"><span>Français</span></a></li><li class="interlanguage-link interwiki-ko mw-list-item"><a href="https://ko.wikipedia.org/wiki/%EC%97%AD%EC%9E%91%EC%9A%A9%EC%A0%9C" title="역작용제 – Korean" lang="ko" hreflang="ko" data-title="역작용제" data-language-autonym="한국어" data-language-local-name="Korean" class="interlanguage-link-target"><span>한국어</span></a></li><li class="interlanguage-link interwiki-hu mw-list-item"><a href="https://hu.wikipedia.org/wiki/Inverz_agonista" title="Inverz agonista – Hungarian" lang="hu" hreflang="hu" data-title="Inverz agonista" data-language-autonym="Magyar" data-language-local-name="Hungarian" class="interlanguage-link-target"><span>Magyar</span></a></li><li class="interlanguage-link interwiki-ja mw-list-item"><a href="https://ja.wikipedia.org/wiki/%E5%8F%97%E5%AE%B9%E4%BD%93%E9%80%86%E4%BD%9C%E5%8B%95%E8%96%AC" title="受容体逆作動薬 – Japanese" lang="ja" hreflang="ja" data-title="受容体逆作動薬" data-language-autonym="日本語" data-language-local-name="Japanese" class="interlanguage-link-target"><span>日本語</span></a></li><li class="interlanguage-link interwiki-pl mw-list-item"><a href="https://pl.wikipedia.org/wiki/Odwrotny_agonista" title="Odwrotny agonista – Polish" lang="pl" hreflang="pl" data-title="Odwrotny agonista" data-language-autonym="Polski" data-language-local-name="Polish" class="interlanguage-link-target"><span>Polski</span></a></li><li class="interlanguage-link interwiki-pt mw-list-item"><a href="https://pt.wikipedia.org/wiki/Agonista_inverso" title="Agonista inverso – Portuguese" lang="pt" hreflang="pt" data-title="Agonista inverso" data-language-autonym="Português" data-language-local-name="Portuguese" class="interlanguage-link-target"><span>Português</span></a></li><li class="interlanguage-link interwiki-ro mw-list-item"><a href="https://ro.wikipedia.org/wiki/Agonist_invers" title="Agonist invers – Romanian" lang="ro" hreflang="ro" data-title="Agonist invers" data-language-autonym="Română" data-language-local-name="Romanian" class="interlanguage-link-target"><span>Română</span></a></li><li class="interlanguage-link interwiki-ru mw-list-item"><a href="https://ru.wikipedia.org/wiki/%D0%9E%D0%B1%D1%80%D0%B0%D1%82%D0%BD%D1%8B%D0%B9_%D0%B0%D0%B3%D0%BE%D0%BD%D0%B8%D1%81%D1%82" title="Обратный агонист – Russian" lang="ru" hreflang="ru" data-title="Обратный агонист" data-language-autonym="Русский" data-language-local-name="Russian" class="interlanguage-link-target"><span>Русский</span></a></li><li class="interlanguage-link interwiki-sr mw-list-item"><a href="https://sr.wikipedia.org/wiki/Inverzni_agonist" title="Inverzni agonist – Serbian" lang="sr" hreflang="sr" data-title="Inverzni agonist" data-language-autonym="Српски / srpski" data-language-local-name="Serbian" class="interlanguage-link-target"><span>Српски / srpski</span></a></li><li class="interlanguage-link interwiki-sh mw-list-item"><a href="https://sh.wikipedia.org/wiki/Inverzni_agonist" title="Inverzni agonist – Serbo-Croatian" lang="sh" hreflang="sh" data-title="Inverzni agonist" data-language-autonym="Srpskohrvatski / српскохрватски" data-language-local-name="Serbo-Croatian" class="interlanguage-link-target"><span>Srpskohrvatski / српскохрватски</span></a></li><li class="interlanguage-link interwiki-fi mw-list-item"><a href="https://fi.wikipedia.org/wiki/K%C3%A4%C3%A4nteisagonisti" title="Käänteisagonisti – Finnish" lang="fi" hreflang="fi" data-title="Käänteisagonisti" data-language-autonym="Suomi" data-language-local-name="Finnish" class="interlanguage-link-target"><span>Suomi</span></a></li><li class="interlanguage-link interwiki-uk mw-list-item"><a href="https://uk.wikipedia.org/wiki/%D0%97%D0%B2%D0%BE%D1%80%D0%BE%D1%82%D0%BD%D0%B8%D0%B9_%D0%B0%D0%B3%D0%BE%D0%BD%D1%96%D1%81%D1%82" title="Зворотний агоніст – Ukrainian" lang="uk" hreflang="uk" data-title="Зворотний агоніст" data-language-autonym="Українська" data-language-local-name="Ukrainian" class="interlanguage-link-target"><span>Українська</span></a></li><li class="interlanguage-link interwiki-vi mw-list-item"><a href="https://vi.wikipedia.org/wiki/Ch%E1%BA%A5t_ch%E1%BB%A7_v%E1%BA%ADn_ngh%E1%BB%8Bch" title="Chất chủ vận nghịch – Vietnamese" lang="vi" hreflang="vi" data-title="Chất chủ vận nghịch" data-language-autonym="Tiếng Việt" data-language-local-name="Vietnamese" class="interlanguage-link-target"><span>Tiếng Việt</span></a></li><li class="interlanguage-link interwiki-zh mw-list-item"><a href="https://zh.wikipedia.org/wiki/%E5%8F%8D%E5%90%91%E6%BF%80%E5%8A%A8%E5%89%82" title="反向激动剂 – Chinese" lang="zh" hreflang="zh" data-title="反向激动剂" data-language-autonym="中文" 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searchaux" style="display:none">Agent in biochemistry</div> <style data-mw-deduplicate="TemplateStyles:r1236090951">.mw-parser-output .hatnote{font-style:italic}.mw-parser-output div.hatnote{padding-left:1.6em;margin-bottom:0.5em}.mw-parser-output .hatnote i{font-style:normal}.mw-parser-output .hatnote+link+.hatnote{margin-top:-0.5em}@media print{body.ns-0 .mw-parser-output .hatnote{display:none!important}}</style><div role="note" class="hatnote navigation-not-searchable">Not to be confused with <a href="/wiki/Antagonist_(disambiguation)" class="mw-disambig" title="Antagonist (disambiguation)">Antagonist</a> or <a href="/wiki/Protagonist_(disambiguation)" class="mw-disambig" title="Protagonist (disambiguation)">Protagonist</a>.</div> <figure typeof="mw:File/Thumb"><a href="/wiki/File:Inverse_agonist_3.svg" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/6/6c/Inverse_agonist_3.svg/400px-Inverse_agonist_3.svg.png" decoding="async" width="400" height="219" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/6/6c/Inverse_agonist_3.svg/600px-Inverse_agonist_3.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/6/6c/Inverse_agonist_3.svg/800px-Inverse_agonist_3.svg.png 2x" data-file-width="534" data-file-height="293" /></a><figcaption>Dose response curves of a full agonist, partial agonist, neutral antagonist, and inverse agonist</figcaption></figure> <p>In <a href="/wiki/Pharmacology" title="Pharmacology">pharmacology</a>, an <b>inverse agonist</b> is a <a href="/wiki/Drug" title="Drug">drug</a> that binds to the same <a href="/wiki/Receptor_(biochemistry)" title="Receptor (biochemistry)">receptor</a> as an <a href="/wiki/Agonist" title="Agonist">agonist</a> but induces a pharmacological response opposite to that of the agonist. </p><p>A <a href="/wiki/Receptor_antagonist" title="Receptor antagonist">neutral antagonist</a> has no activity in the absence of an agonist or inverse agonist but can block the activity of either;<sup id="cite_ref-1" class="reference"><a href="#cite_note-1"><span class="cite-bracket">[</span>1<span class="cite-bracket">]</span></a></sup> they are in fact sometimes called <i>blockers</i> (examples include <a href="/wiki/Alpha_blocker" title="Alpha blocker">alpha blockers</a>, <a href="/wiki/Beta_blocker" title="Beta blocker">beta blockers</a>, and <a href="/wiki/Calcium_channel_blocker" title="Calcium channel blocker">calcium channel blockers</a>). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists.<sup id="cite_ref-pmid27955830_2-0" class="reference"><a href="#cite_note-pmid27955830-2"><span class="cite-bracket">[</span>2<span class="cite-bracket">]</span></a></sup> </p><p>A prerequisite for an inverse agonist response is that the receptor must have a <a href="/wiki/Receptor_(biochemistry)#Constitutive_activity" title="Receptor (biochemistry)">constitutive</a> (also known as <a href="/wiki/Intrinsic_activity" title="Intrinsic activity">intrinsic</a> or basal) level of activity in the absence of any <a href="/wiki/Ligand_(biochemistry)" title="Ligand (biochemistry)">ligand</a>.<sup id="cite_ref-3" class="reference"><a href="#cite_note-3"><span class="cite-bracket">[</span>3<span class="cite-bracket">]</span></a></sup> An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. </p><p>The <a href="/wiki/Efficacy" title="Efficacy">efficacy</a> of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., negative) efficacy. </p> <meta property="mw:PageProp/toc" /> <div class="mw-heading mw-heading2"><h2 id="Examples">Examples</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=1" title="Edit section: Examples"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Receptors for which inverse agonists have been identified include the <a href="/wiki/GABAA" class="mw-redirect" title="GABAA">GABA<sub>A</sub></a>, <a href="/wiki/Melanocortin_receptor" title="Melanocortin receptor">melanocortin</a>, <a href="/wiki/Mu_opioid_receptor" class="mw-redirect" title="Mu opioid receptor">mu opioid</a>, <a href="/wiki/Histamine_receptor" title="Histamine receptor">histamine</a> and <a href="/wiki/Beta_adrenergic_receptor" class="mw-redirect" title="Beta adrenergic receptor">beta adrenergic receptors</a>. Both <a href="/wiki/Endogeny_(biology)" title="Endogeny (biology)">endogenous</a> and <a href="/wiki/Exogeny" title="Exogeny">exogenous</a> inverse agonists have been identified, as have drugs at ligand gated ion channels and at G protein-coupled receptors. </p> <div class="mw-heading mw-heading3"><h3 id="Ligand_gated_ion_channel_inverse_agonists">Ligand gated ion channel inverse agonists</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=2" title="Edit section: Ligand gated ion channel inverse agonists"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>An example of a receptor site that possesses basal activity and for which inverse agonists have been identified is the <a href="/wiki/GABAA_receptors" class="mw-redirect" title="GABAA receptors">GABA<sub>A</sub> receptors</a>. Agonists for GABA<sub>A</sub> receptors (such as <a href="/wiki/Muscimol" title="Muscimol">muscimol</a>) create a <a href="/wiki/Relaxant" class="mw-redirect" title="Relaxant">relaxant</a> effect, whereas inverse agonists have <a href="/wiki/Agitation_(action)" class="mw-redirect" title="Agitation (action)">agitation</a> effects (for example, <a href="/wiki/Ro15-4513" title="Ro15-4513">Ro15-4513</a>) or even <a href="/wiki/Convulsive" class="mw-redirect" title="Convulsive">convulsive</a> and <a href="/wiki/Anxiogenic" title="Anxiogenic">anxiogenic</a> effects (certain <a href="/wiki/Beta-carboline" class="mw-redirect" title="Beta-carboline">beta-carbolines</a>).<sup id="cite_ref-4" class="reference"><a href="#cite_note-4"><span class="cite-bracket">[</span>4<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-5" class="reference"><a href="#cite_note-5"><span class="cite-bracket">[</span>5<span class="cite-bracket">]</span></a></sup> </p> <div class="mw-heading mw-heading3"><h3 id="G_protein-coupled_receptor_inverse_agonists">G protein-coupled receptor inverse agonists</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=3" title="Edit section: G protein-coupled receptor inverse agonists"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Two known endogenous inverse agonists are the <a href="/wiki/Agouti-related_peptide" title="Agouti-related peptide">Agouti-related peptide</a> (AgRP) and its associated peptide <a href="/wiki/Agouti_signalling_peptide" class="mw-redirect" title="Agouti signalling peptide">Agouti signalling peptide</a> (ASIP). AgRP and ASIP appear naturally in humans and bind <a href="/wiki/Melanocortin_receptors" class="mw-redirect" title="Melanocortin receptors">melanocortin receptors</a> 4 and 1 (<a href="/wiki/Melanocortin_4_receptor" title="Melanocortin 4 receptor">Mc4R</a> and <a href="/wiki/Melanocortin_1_receptor" title="Melanocortin 1 receptor">Mc1R</a>), respectively, with nanomolar affinities.<sup id="cite_ref-pmid9450927_6-0" class="reference"><a href="#cite_note-pmid9450927-6"><span class="cite-bracket">[</span>6<span class="cite-bracket">]</span></a></sup> </p><p>The <a href="/wiki/Opioid_antagonist" title="Opioid antagonist">opioid antagonists</a> <a href="/wiki/Naloxone" title="Naloxone">naloxone</a> and <a href="/wiki/Naltrexone" title="Naltrexone">naltrexone</a> act as <a href="/wiki/Receptor_antagonist" title="Receptor antagonist">neutral antagonists</a> of the <a href="/wiki/Mu_opioid_receptors" class="mw-redirect" title="Mu opioid receptors">mu opioid receptors</a> under basal conditions, but as inverse agonists when an opioid such as <a href="/wiki/Morphine" title="Morphine">morphine</a> is bound to the same channel. 6α-naltrexo, <a href="/wiki/6%CE%B2-Naltrexol" title="6β-Naltrexol">6β-naltrexol</a>, 6β-naloxol, and 6β-naltrexamine acted <a href="/wiki/Receptor_antagonist" title="Receptor antagonist">neutral antagonists</a> regardless of opioid binding and caused significantly reduced withdrawal jumping when compared to <a href="/wiki/Naloxone" title="Naloxone">naloxone</a> and <a href="/wiki/Naltrexone" title="Naltrexone">naltrexone</a>.<sup id="cite_ref-pmid11413242_7-0" class="reference"><a href="#cite_note-pmid11413242-7"><span class="cite-bracket">[</span>7<span class="cite-bracket">]</span></a></sup> </p><p>Nearly all antihistamines acting at <a href="/wiki/H1_receptors" class="mw-redirect" title="H1 receptors">H1 receptors</a> and <a href="/wiki/H2_receptors" class="mw-redirect" title="H2 receptors">H2 receptors</a> have been shown to be inverse agonists.<sup id="cite_ref-:0_8-0" class="reference"><a href="#cite_note-:0-8"><span class="cite-bracket">[</span>8<span class="cite-bracket">]</span></a></sup> </p><p>The <a href="/wiki/Beta_blockers" class="mw-redirect" title="Beta blockers">beta blockers</a> <a href="/wiki/Carvedilol" title="Carvedilol">carvedilol</a> and <a href="/wiki/Bucindolol" title="Bucindolol">bucindolol</a> have been shown to be low level inverse agonists at <a href="/wiki/Beta_adrenoceptors" class="mw-redirect" title="Beta adrenoceptors">beta adrenoceptors</a>.<sup id="cite_ref-:0_8-1" class="reference"><a href="#cite_note-:0-8"><span class="cite-bracket">[</span>8<span class="cite-bracket">]</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Mechanisms_of_action">Mechanisms of action</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=4" title="Edit section: Mechanisms of action"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <figure typeof="mw:File/Thumb"><a href="/wiki/File:Basal_activity_of_receptor_changes.png" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/d/d7/Basal_activity_of_receptor_changes.png/431px-Basal_activity_of_receptor_changes.png" decoding="async" width="431" height="369" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/d/d7/Basal_activity_of_receptor_changes.png/647px-Basal_activity_of_receptor_changes.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/d/d7/Basal_activity_of_receptor_changes.png/862px-Basal_activity_of_receptor_changes.png 2x" data-file-width="1074" data-file-height="920" /></a><figcaption>Figure 2: Example of changes in Intrinsic activity based on mutations and the presence of inverse agonists. (assuming the inverse agonist has the same binding affinity for both the normal and mutated receptor)</figcaption></figure> <p>Like <a href="/wiki/Agonist" title="Agonist">agonists</a>, inverse agonists have their own unique ways of inducing pharmacological and physiological responses depending on many factors, such as the type of inverse agonist, the type of <a href="/wiki/Receptor_(biochemistry)" title="Receptor (biochemistry)">receptor</a>, mutants of receptors, binding affinities and whether the effects are exerted acutely or chronically based on receptor population density.<sup id="cite_ref-:2_9-0" class="reference"><a href="#cite_note-:2-9"><span class="cite-bracket">[</span>9<span class="cite-bracket">]</span></a></sup> Because of this, they exhibit a spectrum of activity below the <a href="/wiki/Intrinsic_activity" title="Intrinsic activity">Intrinsic activity</a> level.<sup id="cite_ref-:2_9-1" class="reference"><a href="#cite_note-:2-9"><span class="cite-bracket">[</span>9<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-:1_10-0" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">[</span>10<span class="cite-bracket">]</span></a></sup> Changes in constitutive activity of receptors affect response levels from ligands like inverse agonists.<sup id="cite_ref-11" class="reference"><a href="#cite_note-11"><span class="cite-bracket">[</span>11<span class="cite-bracket">]</span></a></sup> </p><p>To illustrate, mechanistic models have been made for how inverse agonists induce their responses on <a href="/wiki/G_protein-coupled_receptor" title="G protein-coupled receptor">G protein-coupled receptors</a> (GPCRs). Many types of Inverse agonists for <a href="/wiki/G_protein-coupled_receptor" title="G protein-coupled receptor">GPCRs</a> have been shown to exhibit the following conventionally accepted mechanism. </p><p>Based on the Extended <a href="/wiki/Ternary_complex" title="Ternary complex">Ternary complex</a> model, the mechanism contends that inverse agonists switch the receptor from an active state to an inactive state by undergoing conformational changes.<sup id="cite_ref-:02_12-0" class="reference"><a href="#cite_note-:02-12"><span class="cite-bracket">[</span>12<span class="cite-bracket">]</span></a></sup> Under this model, current thinking is that the <a href="/wiki/G_protein-coupled_receptor" title="G protein-coupled receptor">GPCRs</a> can exist in a continuum of active and inactive states when no ligand is present.<sup id="cite_ref-:02_12-1" class="reference"><a href="#cite_note-:02-12"><span class="cite-bracket">[</span>12<span class="cite-bracket">]</span></a></sup> Inverse agonists stabilize the inactive states, thereby suppressing agonist-independent activity.<sup id="cite_ref-:02_12-2" class="reference"><a href="#cite_note-:02-12"><span class="cite-bracket">[</span>12<span class="cite-bracket">]</span></a></sup> However, the implementation of 'constitutively active mutants'<sup id="cite_ref-:02_12-3" class="reference"><a href="#cite_note-:02-12"><span class="cite-bracket">[</span>12<span class="cite-bracket">]</span></a></sup> of <a href="/wiki/G_protein-coupled_receptor" title="G protein-coupled receptor">GPCRs</a> change their intrinsic activity.<sup id="cite_ref-:2_9-2" class="reference"><a href="#cite_note-:2-9"><span class="cite-bracket">[</span>9<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-:1_10-1" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">[</span>10<span class="cite-bracket">]</span></a></sup> Thus, the effect an inverse agonist has on a receptor depends on the basal activity of the receptor, assuming the inverse agonist has the same binding affinity (as shown in the figure 2). </p> <div class="mw-heading mw-heading2"><h2 id="See_also">See also</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=5" title="Edit section: See also"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <ul><li><a href="/wiki/Agonist" title="Agonist">Agonist</a></li> <li><a href="/wiki/Receptor_antagonist" title="Receptor antagonist">Receptor antagonist</a></li> <li><a href="/wiki/Autoreceptor" title="Autoreceptor">Autoreceptor</a></li></ul> <div class="mw-heading mw-heading2"><h2 id="References">References</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=6" title="Edit section: References"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <style data-mw-deduplicate="TemplateStyles:r1239543626">.mw-parser-output .reflist{margin-bottom:0.5em;list-style-type:decimal}@media screen{.mw-parser-output .reflist{font-size:90%}}.mw-parser-output .reflist .references{font-size:100%;margin-bottom:0;list-style-type:inherit}.mw-parser-output .reflist-columns-2{column-width:30em}.mw-parser-output .reflist-columns-3{column-width:25em}.mw-parser-output .reflist-columns{margin-top:0.3em}.mw-parser-output .reflist-columns ol{margin-top:0}.mw-parser-output .reflist-columns li{page-break-inside:avoid;break-inside:avoid-column}.mw-parser-output .reflist-upper-alpha{list-style-type:upper-alpha}.mw-parser-output .reflist-upper-roman{list-style-type:upper-roman}.mw-parser-output .reflist-lower-alpha{list-style-type:lower-alpha}.mw-parser-output .reflist-lower-greek{list-style-type:lower-greek}.mw-parser-output .reflist-lower-roman{list-style-type:lower-roman}</style><div class="reflist"> <div class="mw-references-wrap mw-references-columns"><ol 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a{background:url("//upload.wikimedia.org/wikipedia/commons/4/4c/Wikisource-logo.svg")right 0.1em center/12px no-repeat}body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-free a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-limited a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-registration a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-subscription a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .cs1-ws-icon a{background-size:contain;padding:0 1em 0 0}.mw-parser-output .cs1-code{color:inherit;background:inherit;border:none;padding:inherit}.mw-parser-output .cs1-hidden-error{display:none;color:var(--color-error,#d33)}.mw-parser-output .cs1-visible-error{color:var(--color-error,#d33)}.mw-parser-output .cs1-maint{display:none;color:#085;margin-left:0.3em}.mw-parser-output .cs1-kern-left{padding-left:0.2em}.mw-parser-output .cs1-kern-right{padding-right:0.2em}.mw-parser-output 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(2004-01-05). <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/14722344/">"Inverse agonists: tools to reveal ligand-specific conformations of G protein-coupled receptors"</a>. <i>Science's STKE: Signal Transduction Knowledge Environment</i>. <b>2004</b> (215): pe1. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1126%2Fstke.2152004pe1">10.1126/stke.2152004pe1</a>. <a href="/wiki/ISSN_(identifier)" class="mw-redirect" title="ISSN (identifier)">ISSN</a> <a rel="nofollow" class="external text" href="https://search.worldcat.org/issn/1525-8882">1525-8882</a>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a> <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/14722344">14722344</a>. <a href="/wiki/S2CID_(identifier)" class="mw-redirect" title="S2CID (identifier)">S2CID</a> <a rel="nofollow" class="external text" href="https://api.semanticscholar.org/CorpusID:22336235">22336235</a>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Science%27s+STKE%3A+Signal+Transduction+Knowledge+Environment&rft.atitle=Inverse+agonists%3A+tools+to+reveal+ligand-specific+conformations+of+G+protein-coupled+receptors&rft.volume=2004&rft.issue=215&rft.pages=pe1&rft.date=2004-01-05&rft.issn=1525-8882&rft_id=https%3A%2F%2Fapi.semanticscholar.org%2FCorpusID%3A22336235%23id-name%3DS2CID&rft_id=info%3Apmid%2F14722344&rft_id=info%3Adoi%2F10.1126%2Fstke.2152004pe1&rft.aulast=Prather&rft.aufirst=Paul+L.&rft_id=https%3A%2F%2Fpubmed.ncbi.nlm.nih.gov%2F14722344%2F&rfr_id=info%3Asid%2Fen.wikipedia.org%3AInverse+agonist" class="Z3988"></span></span> </li> <li id="cite_note-:1-10"><span class="mw-cite-backlink">^ <a href="#cite_ref-:1_10-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-:1_10-1"><sup><i><b>b</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFHirayamaFujii2020" class="citation journal cs1">Hirayama, Shigeto; Fujii, Hideaki (2020). <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/32238139/">"δ Opioid Receptor Inverse Agonists and their In Vivo Pharmacological Effects"</a>. <i>Current Topics in Medicinal Chemistry</i>. <b>20</b> (31): <span class="nowrap">2889–</span>2902. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.2174%2F1568026620666200402115654">10.2174/1568026620666200402115654</a>. <a href="/wiki/ISSN_(identifier)" class="mw-redirect" title="ISSN (identifier)">ISSN</a> <a rel="nofollow" class="external text" href="https://search.worldcat.org/issn/1873-4294">1873-4294</a>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a> <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/32238139">32238139</a>. <a href="/wiki/S2CID_(identifier)" class="mw-redirect" title="S2CID (identifier)">S2CID</a> <a rel="nofollow" class="external text" href="https://api.semanticscholar.org/CorpusID:214767114">214767114</a>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Current+Topics+in+Medicinal+Chemistry&rft.atitle=%CE%B4+Opioid+Receptor+Inverse+Agonists+and+their+In+Vivo+Pharmacological+Effects&rft.volume=20&rft.issue=31&rft.pages=%3Cspan+class%3D%22nowrap%22%3E2889-%3C%2Fspan%3E2902&rft.date=2020&rft.issn=1873-4294&rft_id=https%3A%2F%2Fapi.semanticscholar.org%2FCorpusID%3A214767114%23id-name%3DS2CID&rft_id=info%3Apmid%2F32238139&rft_id=info%3Adoi%2F10.2174%2F1568026620666200402115654&rft.aulast=Hirayama&rft.aufirst=Shigeto&rft.au=Fujii%2C+Hideaki&rft_id=https%3A%2F%2Fpubmed.ncbi.nlm.nih.gov%2F32238139%2F&rfr_id=info%3Asid%2Fen.wikipedia.org%3AInverse+agonist" class="Z3988"></span></span> </li> <li id="cite_note-11"><span class="mw-cite-backlink"><b><a href="#cite_ref-11">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFBergClarke2018" class="citation journal cs1">Berg, Kelly A.; Clarke, William P. (2018-10-01). <a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6165953">"Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity"</a>. <i>The International Journal of Neuropsychopharmacology</i>. <b>21</b> (10): <span class="nowrap">962–</span>977. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1093%2Fijnp%2Fpyy071">10.1093/ijnp/pyy071</a>. <a href="/wiki/ISSN_(identifier)" class="mw-redirect" title="ISSN (identifier)">ISSN</a> <a rel="nofollow" class="external text" href="https://search.worldcat.org/issn/1469-5111">1469-5111</a>. <a href="/wiki/PMC_(identifier)" class="mw-redirect" title="PMC (identifier)">PMC</a> <span class="id-lock-free" title="Freely accessible"><a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6165953">6165953</a></span>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a> <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/30085126">30085126</a>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=The+International+Journal+of+Neuropsychopharmacology&rft.atitle=Making+Sense+of+Pharmacology%3A+Inverse+Agonism+and+Functional+Selectivity&rft.volume=21&rft.issue=10&rft.pages=%3Cspan+class%3D%22nowrap%22%3E962-%3C%2Fspan%3E977&rft.date=2018-10-01&rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC6165953%23id-name%3DPMC&rft.issn=1469-5111&rft_id=info%3Apmid%2F30085126&rft_id=info%3Adoi%2F10.1093%2Fijnp%2Fpyy071&rft.aulast=Berg&rft.aufirst=Kelly+A.&rft.au=Clarke%2C+William+P.&rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC6165953&rfr_id=info%3Asid%2Fen.wikipedia.org%3AInverse+agonist" class="Z3988"></span></span> </li> <li id="cite_note-:02-12"><span class="mw-cite-backlink">^ <a href="#cite_ref-:02_12-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-:02_12-1"><sup><i><b>b</b></i></sup></a> <a href="#cite_ref-:02_12-2"><sup><i><b>c</b></i></sup></a> <a href="#cite_ref-:02_12-3"><sup><i><b>d</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFStrange2002" class="citation journal cs1">Strange, Philip G. (February 2002). <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/11830266/">"Mechanisms of inverse agonism at G-protein-coupled receptors"</a>. <i>Trends in Pharmacological Sciences</i>. <b>23</b> (2): <span class="nowrap">89–</span>95. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1016%2Fs0165-6147%2802%2901993-4">10.1016/s0165-6147(02)01993-4</a>. <a href="/wiki/ISSN_(identifier)" class="mw-redirect" title="ISSN (identifier)">ISSN</a> <a rel="nofollow" class="external text" href="https://search.worldcat.org/issn/0165-6147">0165-6147</a>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a> <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/11830266">11830266</a>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Trends+in+Pharmacological+Sciences&rft.atitle=Mechanisms+of+inverse+agonism+at+G-protein-coupled+receptors&rft.volume=23&rft.issue=2&rft.pages=%3Cspan+class%3D%22nowrap%22%3E89-%3C%2Fspan%3E95&rft.date=2002-02&rft.issn=0165-6147&rft_id=info%3Apmid%2F11830266&rft_id=info%3Adoi%2F10.1016%2Fs0165-6147%2802%2901993-4&rft.aulast=Strange&rft.aufirst=Philip+G.&rft_id=https%3A%2F%2Fpubmed.ncbi.nlm.nih.gov%2F11830266%2F&rfr_id=info%3Asid%2Fen.wikipedia.org%3AInverse+agonist" class="Z3988"></span></span> </li> </ol></div></div> <div class="mw-heading mw-heading2"><h2 id="External_links">External links</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Inverse_agonist&action=edit&section=7" title="Edit section: External links"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <ul><li><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFJeffries_WB1999" class="citation web cs1">Jeffries WB (1999-02-17). <a rel="nofollow" class="external text" href="https://medicine.creighton.edu/courses/pharm/Dr.Jeffries/Inverse.asp">"Inverse Agonists for Medical Students"</a>. <i>Office of Medical Education - Courses - IDC 105 Principles of Pharmacology</i>. Creighton University School of Medicine - Department of Pharmacology<span class="reference-accessdate">. Retrieved <span class="nowrap">2008-08-12</span></span>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=unknown&rft.jtitle=Office+of+Medical+Education+-+Courses+-+IDC+105+Principles+of+Pharmacology&rft.atitle=Inverse+Agonists+for+Medical+Students&rft.date=1999-02-17&rft.au=Jeffries+WB&rft_id=https%3A%2F%2Fmedicine.creighton.edu%2Fcourses%2Fpharm%2FDr.Jeffries%2FInverse.asp&rfr_id=info%3Asid%2Fen.wikipedia.org%3AInverse+agonist" class="Z3988"></span><sup class="noprint Inline-Template"><span style="white-space: nowrap;">[<i><a href="/wiki/Wikipedia:Link_rot" title="Wikipedia:Link rot"><span title=" Dead link tagged March 2022">permanent dead link</span></a></i><span style="visibility:hidden; color:transparent; padding-left:2px">‍</span>]</span></sup></li> <li><a rel="nofollow" class="external text" href="http://pharmacologycorner.com/inverse-agonists/">Inverse Agonists: An Illustrated Tutorial</a> Panesar K, Guzman F. Pharmacology Corner. 2012</li></ul> <div class="navbox-styles"><style data-mw-deduplicate="TemplateStyles:r1129693374">.mw-parser-output .hlist dl,.mw-parser-output .hlist ol,.mw-parser-output .hlist ul{margin:0;padding:0}.mw-parser-output .hlist dd,.mw-parser-output .hlist dt,.mw-parser-output .hlist li{margin:0;display:inline}.mw-parser-output .hlist.inline,.mw-parser-output .hlist.inline dl,.mw-parser-output .hlist.inline ol,.mw-parser-output .hlist.inline ul,.mw-parser-output .hlist dl dl,.mw-parser-output .hlist dl ol,.mw-parser-output .hlist dl ul,.mw-parser-output .hlist ol dl,.mw-parser-output .hlist ol ol,.mw-parser-output .hlist ol ul,.mw-parser-output .hlist ul dl,.mw-parser-output .hlist ul ol,.mw-parser-output .hlist ul ul{display:inline}.mw-parser-output .hlist .mw-empty-li{display:none}.mw-parser-output .hlist dt::after{content:": "}.mw-parser-output .hlist dd::after,.mw-parser-output .hlist li::after{content:" · ";font-weight:bold}.mw-parser-output .hlist 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href="/wiki/Ligand_(biochemistry)" title="Ligand (biochemistry)">Ligand (biochemistry)</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Excitatory10" scope="row" class="navbox-group" style="width:1%;text-align: center;">Excitatory</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Agonist" title="Agonist">Agonist</a></li> <li><a href="/wiki/Endogenous_agonist" title="Endogenous agonist">Endogenous agonist</a></li> <li><a href="/wiki/Irreversible_agonist" title="Irreversible agonist">Irreversible agonist</a></li> <li><a href="/wiki/Partial_agonist" title="Partial agonist">Partial agonist</a></li> <li><a href="/wiki/Superagonist" title="Superagonist">Superagonist</a></li> <li><a href="/wiki/Physiological_agonism_and_antagonism" title="Physiological agonism and antagonism">Physiological agonist</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Inhibitory10" scope="row" class="navbox-group" style="width:1%;text-align: center;">Inhibitory</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Receptor_antagonist" title="Receptor antagonist">Antagonist</a></li> <li><a href="/wiki/Competitive_antagonist" class="mw-redirect" title="Competitive antagonist">Competitive antagonist</a></li> <li><a href="/wiki/Irreversible_antagonist" title="Irreversible antagonist">Irreversible antagonist</a></li> <li><a href="/wiki/Physiological_agonism_and_antagonism" title="Physiological agonism and antagonism">Physiological antagonist</a></li> <li><a class="mw-selflink selflink">Inverse agonist</a></li> <li><a href="/wiki/Enzyme_inhibitor" title="Enzyme inhibitor">Enzyme inhibitor</a></li></ul> </div></td></tr></tbody></table><div> <ul><li><a href="/wiki/Drug" title="Drug">Drug</a></li> <li><a href="/wiki/Neurotransmitter" title="Neurotransmitter">Neurotransmitter</a></li> <li><a href="/wiki/Agonist-antagonist" title="Agonist-antagonist">Agonist-antagonist</a></li> <li><a href="/wiki/Pharmacophore" title="Pharmacophore">Pharmacophore</a></li></ul></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Pharmacodynamics" title="Pharmacodynamics">Pharmacodynamics</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Activity_at_receptor20" scope="row" class="navbox-group" style="width:1%;text-align: center;">Activity at receptor</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <li><a href="/wiki/Mechanism_of_action" title="Mechanism of action">Mechanism of action</a></li> <li><a href="/wiki/Mode_of_action" title="Mode of action">Mode of action</a></li> <li><a href="/wiki/Molecular_binding" title="Molecular binding">Binding</a></li> <li><a href="/wiki/Receptor_(biochemistry)" title="Receptor (biochemistry)">Receptor (biochemistry)</a></li> <li><a href="/wiki/Desensitization_(medicine)" title="Desensitization (medicine)">Desensitization (medicine)</a></li> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Other_effects_of_ligand23" scope="row" class="navbox-group" style="width:1%;text-align: center;">Other effects of ligand</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li>Selectivity (<a href="/wiki/Binding_selectivity" title="Binding selectivity">Binding</a>, <a href="/wiki/Functional_selectivity" title="Functional selectivity">Functional</a>)</li> <li><a href="/wiki/Pleiotropy_(drugs)" title="Pleiotropy (drugs)">Pleiotropy (drugs)</a></li> <li><a href="/wiki/Non-specific_effect_of_vaccines" title="Non-specific effect of vaccines">Non-specific effect of vaccines</a></li> <li><a href="/wiki/Adverse_effect" title="Adverse effect">Adverse effect</a></li> <li><a href="/wiki/Toxicity" title="Toxicity">Toxicity</a> (<a href="/wiki/Neurotoxicity" title="Neurotoxicity">Neurotoxicity</a>)</li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Analysis8" scope="row" class="navbox-group" style="width:1%;text-align: center;">Analysis</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Dose%E2%80%93response_relationship" title="Dose–response relationship">Dose–response relationship</a></li> <li><a href="/wiki/Hill_equation_(biochemistry)" title="Hill equation (biochemistry)">Hill equation (biochemistry)</a></li> <li><a href="/wiki/Schild_plot" class="mw-redirect" title="Schild plot">Schild plot</a></li> <li><a href="/wiki/Del_Castillo_Katz_model" class="mw-redirect" title="Del Castillo Katz model">Del Castillo Katz model</a></li> <li><a href="/wiki/Cheng-Prussoff_Equation" class="mw-redirect" title="Cheng-Prussoff Equation">Cheng-Prussoff Equation</a></li> <li>Methods (<a href="/wiki/Organ_bath" title="Organ bath">Organ bath</a>, <a href="/wiki/Ligand_binding_assay" title="Ligand binding assay">Ligand binding assay</a>, <a href="/wiki/Patch_clamp" title="Patch clamp">Patch clamp</a>)</li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Metrics7" scope="row" class="navbox-group" style="width:1%;text-align: center;">Metrics</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Efficacy#Pharmacology" title="Efficacy">Efficacy</a></li> <li><a href="/wiki/Intrinsic_activity" title="Intrinsic activity">Intrinsic activity</a></li> <li><a href="/wiki/Potency_(pharmacology)" title="Potency (pharmacology)">Potency</a> (<a href="/wiki/EC50" title="EC50">EC50</a>, <a href="/wiki/IC50" title="IC50">IC50</a>, <a href="/wiki/Effective_dose_(pharmacology)" title="Effective dose (pharmacology)">ED50</a>, <a href="/wiki/Median_lethal_dose" title="Median lethal dose">LD50</a>, <a href="/wiki/Median_toxic_dose" title="Median toxic dose">TD50</a>)</li> <li><a href="/wiki/Therapeutic_index" title="Therapeutic index">Therapeutic index</a></li> <li><a href="/wiki/Dissociation_constant#Protein-ligand_binding" title="Dissociation constant">Affinity</a></li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Pharmacokinetics" title="Pharmacokinetics">Pharmacokinetics</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Metrics7" scope="row" class="navbox-group" style="width:1%;text-align: center;">Metrics</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Loading_dose" title="Loading dose">Loading dose</a></li> <li><a href="/wiki/Volume_of_distribution" title="Volume of distribution">Volume of distribution</a> (<a href="/wiki/Initial_volume_of_distribution" title="Initial volume of distribution">Initial</a>)</li> <li><a href="/wiki/Rate_of_infusion" title="Rate of infusion">Rate of infusion</a></li> <li><a href="/wiki/Onset_of_action" title="Onset of action">Onset of action</a></li> <li><a href="/wiki/Biological_half-life" title="Biological half-life">Biological half-life</a></li> <li><a href="/wiki/Plasma_protein_binding" title="Plasma protein binding">Plasma protein binding</a></li> <li><a href="/wiki/Bioavailability" title="Bioavailability">Bioavailability</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="LADME5" scope="row" class="navbox-group" style="width:1%;text-align: center;">LADME</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/ADME" title="ADME">(L)ADME</a>: (<a href="/wiki/Liberation_(pharmacology)" title="Liberation (pharmacology)">Liberation</a>)</li> <li><a href="/wiki/Absorption_(pharmacology)" title="Absorption (pharmacology)">Absorption</a></li> <li><a href="/wiki/Distribution_(pharmacology)" title="Distribution (pharmacology)">Distribution</a></li> <li><a href="/wiki/Drug_metabolism" title="Drug metabolism">Metabolism</a></li> <li><a href="/wiki/Excretion" title="Excretion">Excretion</a> (<a href="/wiki/Clearance_(pharmacology)" title="Clearance (pharmacology)">Clearance</a>)</li></ul> </div></td></tr></tbody></table><div> <ul><li><a href="/wiki/Compartment_(pharmacokinetics)" title="Compartment (pharmacokinetics)">Compartment</a></li> <li><a href="/wiki/Bioequivalence" title="Bioequivalence">Bioequivalence</a></li></ul></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;">Related<br /> fields</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Neuroscience_and_psychology35" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Neuroscience" title="Neuroscience">Neuroscience</a> and <a href="/wiki/Psychology" title="Psychology">psychology</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <li><a href="/wiki/Neuropsychopharmacology" title="Neuropsychopharmacology">Neuropsychopharmacology</a></li> <li><a href="/wiki/Neuropharmacology" title="Neuropharmacology">Neuropharmacology</a></li> <li><a href="/wiki/Psychopharmacology" title="Psychopharmacology">Psychopharmacology</a></li> <li><a href="/wiki/Electrophysiology" title="Electrophysiology">Electrophysiology</a></li> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Medicine12" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Medicine" title="Medicine">Medicine</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Clinical_pharmacology" title="Clinical pharmacology">Clinical pharmacology</a></li> <li><a href="/wiki/Pharmacy" title="Pharmacy">Pharmacy</a></li> <li><a href="/wiki/Medicinal_chemistry" title="Medicinal chemistry">Medicinal chemistry</a></li> <li><a href="/wiki/Pharmacoepidemiology" title="Pharmacoepidemiology">Pharmacoepidemiology</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Biochemistry_and_genetics33" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Biochemistry" title="Biochemistry">Biochemistry</a> and <a href="/wiki/Genetics" title="Genetics">genetics</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Pharmacoinformatics" title="Pharmacoinformatics">Pharmacoinformatics</a></li> <li><a href="/wiki/Pharmacogenetics" class="mw-redirect" title="Pharmacogenetics">Pharmacogenetics</a></li> <li><a href="/wiki/Pharmacogenomics" title="Pharmacogenomics">Pharmacogenomics</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Toxicology14" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Toxicology" title="Toxicology">Toxicology</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Pharmacotoxicology" title="Pharmacotoxicology">Pharmacotoxicology</a></li> <li><a href="/wiki/Neurotoxicology" class="mw-redirect" title="Neurotoxicology">Neurotoxicology</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Drug_discovery18" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Drug_discovery" title="Drug discovery">Drug discovery</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Classical_pharmacology" title="Classical pharmacology">Classical pharmacology</a></li> <li><a href="/wiki/Reverse_pharmacology" title="Reverse pharmacology">Reverse pharmacology</a></li></ul> </div></td></tr></tbody></table><div> <ul><li><a href="/wiki/Photopharmacology" title="Photopharmacology">Photopharmacology</a></li> <li><a href="/wiki/Immunopharmacology" class="mw-redirect" title="Immunopharmacology">Immunopharmacology</a></li> <li><a href="/wiki/Cell_biology" title="Cell biology">Cell biology</a></li> <li><a href="/wiki/Physiology" title="Physiology">Physiology</a></li></ul></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;">Other</th><td class="navbox-list-with-group navbox-list navbox-even hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"> <li><a href="/wiki/Coinduction_(anesthetics)" title="Coinduction (anesthetics)">Coinduction (anesthetics)</a></li> <li><a href="/wiki/Combination_therapy" title="Combination therapy">Combination therapy</a></li> <li><a href="/wiki/Functional_analog_(chemistry)" title="Functional analog (chemistry)">Functional analog (chemistry)</a></li> <li><a href="/wiki/Polypharmacology" title="Polypharmacology">Polypharmacology</a></li> <li><a href="/wiki/Chemotherapy" title="Chemotherapy">Chemotherapy</a></li> <li><a href="/wiki/Lists_of_drugs" title="Lists of drugs">Lists of drugs</a></li> <li><a href="/wiki/WHO_list_of_essential_medicines" class="mw-redirect" title="WHO list of essential medicines">WHO list of essential medicines</a></li> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Tolerance_and_resistance24" scope="row" class="navbox-group" style="width:1%;text-align: center;">Tolerance and resistance</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Drug_tolerance" title="Drug tolerance">Drug tolerance</a></li> <li><a href="/wiki/Tachyphylaxis" title="Tachyphylaxis">Tachyphylaxis</a></li> <li><a href="/wiki/Drug_resistance" title="Drug resistance">Drug resistance</a></li> <li><a href="/wiki/Antibiotic_resistance" class="mw-redirect" title="Antibiotic resistance">Antibiotic resistance</a></li> <li><a href="/wiki/Multiple_drug_resistance" title="Multiple drug resistance">Multiple drug resistance</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Antimicrobial_pharmacology26" scope="row" class="navbox-group" style="width:1%;text-align: center;">Antimicrobial 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class="vector-icon mw-ui-icon-wikimedia-history mw-ui-icon-wikimedia-wikimedia-history"></span> <span></span> </a> <a href="#" class="cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--icon-only mw-watchlink" id="ca-watchstar-sticky-header" tabindex="-1" data-event-name="watch-sticky-header"><span class="vector-icon mw-ui-icon-wikimedia-star mw-ui-icon-wikimedia-wikimedia-star"></span> <span></span> </a> <a href="#" class="cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--icon-only" id="ca-edit-sticky-header" tabindex="-1" data-event-name="wikitext-edit-sticky-header"><span class="vector-icon mw-ui-icon-wikimedia-wikiText mw-ui-icon-wikimedia-wikimedia-wikiText"></span> <span></span> </a> <a href="#" class="cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--icon-only" id="ca-ve-edit-sticky-header" tabindex="-1" data-event-name="ve-edit-sticky-header"><span class="vector-icon mw-ui-icon-wikimedia-edit mw-ui-icon-wikimedia-wikimedia-edit"></span> <span></span> </a> <a href="#" class="cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--icon-only" id="ca-viewsource-sticky-header" tabindex="-1" data-event-name="ve-edit-protected-sticky-header"><span class="vector-icon mw-ui-icon-wikimedia-editLock mw-ui-icon-wikimedia-wikimedia-editLock"></span> <span></span> </a> </div> <div class="vector-sticky-header-buttons"> <button class="cdx-button cdx-button--weight-quiet mw-interlanguage-selector" id="p-lang-btn-sticky-header" tabindex="-1" data-event-name="ui.dropdown-p-lang-btn-sticky-header"><span class="vector-icon mw-ui-icon-wikimedia-language mw-ui-icon-wikimedia-wikimedia-language"></span> <span>18 languages</span> </button> <a href="#" class="cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--action-progressive" id="ca-addsection-sticky-header" tabindex="-1" data-event-name="addsection-sticky-header"><span class="vector-icon mw-ui-icon-speechBubbleAdd-progressive mw-ui-icon-wikimedia-speechBubbleAdd-progressive"></span> <span>Add topic</span> </a> </div> <div class="vector-sticky-header-icon-end"> <div class="vector-user-links"> </div> </div> </div> </div> </div> <div class="vector-settings" id="p-dock-bottom"> <ul></ul> 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